Synthetic fluorescein‐labeled amphiphilic peptides composed of the hydrophobic cell surface (cs) GRP78‐targeting and hydrophilic, polycationic arginine‐rich cell penetrating peptides demonstrated GRP78‐dependent cell uptake in the DU145 prostate cancer cells, and to a lesser extent in the non‐cancerous human lung fibroblast WI‐38 cell line. The gene discussed is HSPA5; the disease is Familial prostate cancer.